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Improvement and Application of Acute Blood Stasis Rat Model Aligned with the 3Rs (Reduction, Refinement and Replacement) of Humane Animal Experimentation

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Chinese Journal of Integrative Medicine 2020年第4期26卷 292-298页

作者： HUANG Shuai XU Feng WANG Yin-ye shang ming-ying WANG Chao-qun WANG Xuan CAI Shao-qing State Key Laboratory of Natural and Biomimetic Drugs Peking UniversityBeijing(100191)China Hubei Engineering Research Center of Viral Vector Wuhan University of BioengineeringWuhan(430415)China Department of Molecular and Cellular Pharmacology School of Pharmaceutical SciencesPeking UniversityBeijing(100191)China Division of Pharmaceutical Analysis School of Pharmaceutical SciencesPeking UniversityBeijing(100191)China

Objective:To establish a novel cardiocentesis method for withdrawing venous blood from the right atrium,and to improve an acute blood stasis rat model using an ice bath and epinephrine hydrochloride(Epi)while considering the 3Rs(reduction,refinement,and replacement)of humane animal ***:An acute blood stasis model was established in male Sprague-Dawley rats by subcutaneous injection(s.c.)Epi(1.2mg/kg)administration at 0h,followed by a 5-min exposure to an ice-bath at 2h and *** administration at *** rats received physiological *** were fasted overnight and treated with Angelicae Sinensis Lateralis Radix(ASLR)and Pheretima the following *** blood was collected using our novel cardiocentesis method and used to test whole blood viscosity(WBV),prothrombin time(PT),activated partial thromboplastin time(APTT),and fibrinogen(FIB)***:The rats survived the novel cardiocentesis technique;WBV value returned to normal while hematological parameters such as hemoglobin level and red blood cell count were restored to>94%of the corresponding values in normal rats following a 14-day ***(1.2 mg/kg,s.c.)combined with a 5-min exposure to the ice bath replicated the acute blood stasis rat model and was associated with the highest WBV *** rats showing acute blood stasis,ASLR treatment[4g/(kg-d)for 8 days]decreased WBV by 9.98%,11.09%,9.34%,9.00%,7.66%,and 7.03%(P<0.05),while Pheretima treatment[2.6g/(kg?d),for 8 days]decreased WBV by 25.49%,25.94%,16.28%,17.76%,11.07%,and 7.89%(P<0.01)at shear rates of 1,3,10,30,100,and 180 s'1,***,Pheretima treatment increased APTT significantly(P<0.01).Conclusions:We presented a stable,reproducible,and improved acute blood stasis rat model,which could be applied to screen drugs for promoting blood circulation and eliminating blood stasis.

关键词： acute blood stasis rat model cardiocentesis whole blood viscosity coagulation parameters Angelicae Sinensis Lateralis Radix Pheretima Chinese medicine syndrome

Lignans and diterpenes isolated from Tirpitzia ovoidea and their biological activities

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Chinese Journal of Natural Medicines 2017年第12期15卷 938-943页

作者： YANG Xue-Yan ZHANG Yi-Fan LIU Li-Jia WANG Yi shang ming-ying XU Feng LIU Guang-Xue CAI Shao-Qing Department of Natural Medicine School of Pharmaceutical Sciences Peking University Health Science Center Beijing 100191China

A new lignan, tirpitzin A(17) together with 20 known compounds(1-16, and 18-21) were isolated from the ethyl acetate soluble fraction of ethanol extract of the aerial parts of Tirpitzia ovoidea. The structure of new compound was elucidated by means of spectroscopic analysis. Of the known compounds, 7-21 were isolated from Linaceae family for the first time. The pharmacological activity of the crude extracts was tested using a mouse inflammation model induced by dimethyl benzene. The results demonstrated that the ethyl acetate soluble fraction had anti-inflammatory activity. Moreover, the cytotoxic and anti-inflammatory activities of some compounds were studied. The new compound 17 showed moderate cytotoxic effect against Bx PC-3 cell line(IC_50 = 19.51μmol·L^(-1)) and Compound 10 showed significant cytotoxicity against Hep G2, HL-60, U87 and Bx PC-3 cell lines with IC_50 values in the range 4.2-8.3μmol·L^(-1). Additionally, Compounds 2, 10, 11, and 13 exhibited potent inhibitory effects on LPS-induced nitric oxide production in RAW 264.7 macrophages at the concentration of 50μmol·L^(-1).

关键词： Tirpitzia ovoidea Linaceae Lignans Diterpenes Cytotoxic activity Anti-inflammatory activity

Analysis of aristolochic acids, aristololactams and their analogues using liquid chromatography tandem mass spectrometry

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Chinese Journal of Natural Medicines 2016年第8期14卷 626-640页

作者： YU Jie MA Chao-Mei WANG Xuan shang ming-ying Masao Hattori XU Feng JING Yu DONG Shi-Wen XU Yu-Qiong ZHANG Cui-ying CAI Shao-Qing State Key Laboratory of Natural and Biomimetic Drugs School of Pharmaceutical Sciences Peking University Yunnan University of Traditional Chinese Medicine Institute of Natural Medicine University of Toyama School of Life Sciences Inner Mongolia University

More than 80 aristolochic acids(AAs) and aristololactams(ALs) have been found in plants of the Aristolochiaceae family, but relatively few have been fully studied. The present study aimed at developing and validating a liquid chromatography tandem mass spectrometry(LC/MS^n) for the analysis of these compounds. We characterized the fragmentation behaviors of 31 AAs, ALs, and their analogues via high performance liquid chromatography coupled with electrospray ionization mass spectrometry. We summarized their fragmentation rules and used these rules to identify the constituents contained in Aristolochia contorta, Ar. debilis, Ar. manshurensis, Ar. fangchi, Ar. cinnabarina, and Ar. mollissima. The AAs and ALs showed very different MS behaviors. In MS1 of AAs, the characteristic pseudomolecular ions were [M + NH_4]^+, [M + H]^+, and [M + H - H_2O]^+. However, only [M + H]^+ was found in the MS1 of ALs, which was simpler than that of AAs. Distinct MSn fragmentation patterns were found for AAs and ALs, showing the same skeleton among the different substituent groups. The distribution of the 31 constituents in the 6 species of Aristolochia genus was reported for the first time. 25 Analogues of AAs and ALs were detected in this genus. A hierarchical schemes and a calculating formula of the molecular formula of these nitrophenanthrene carboxylic acids and their lactams were proposed. In conclusion, this method could be applied to identification of similar unknown constituents in other plants.

关键词： LC/MS^n Aristolochic acids Aristololactams Fragmentation rules Aristolochia genus

Profiling the metabolites of astrapterocarpan in rat hepatic 9000g supernatant

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Chinese Journal of Natural Medicines 2019年第11期17卷 842-857页

作者： ZHANG Ya-Zhou XU Feng DONG Jing LIANG Jing HASHI Yuki LIU Guang-Xue LI Yao-Li shang ming-ying WANG Xuan CAI Shao-Qing State Key Laboratory of Natural and Biomimetic Drugs School of Pharmaceutical SciencesPeking UniversityBeijing 10000China School of Pharmaceutical Sciences Guizhou UniversityGuiyang 550000China Shimadzu China MS Center Beijing 10000China

Astrapterocarpan(AP) is a bioactive constituent of Astragali Radix and was selected as a model compound for investigating the in vitro metabolism of pterocarpans in this study. Its in vitro metabolism was conducted by incubation with rat hepatic 9000 g supernatant(S9) in the presence of an NADPH-generating system. At first, four compounds were isolated and their structures were elucidated as 6 a-hydroxy-AP(M1), astrametabolin I [M2, 1 a-hydroxy-9, 10-dimethoxy-pterocarp-1(2), 4-diene-3-one], 9-demethyl-AP(M3, nissolin) and 4-methoxy-astraisoflavan(M4, 7, 2’-dihydroxy-4, 3’, 4’-trimethoxy-isoflavan) on the basis of NMR data, respectively. Among them, M1, M2 and M4 were new compounds. Next, the metabolite profile of AP in rat hepatic S9 was obtained via HPLC-DAD-ESI-IT-TOF-MSn, and 40 new metabolites were tentatively identified. These newly identified metabolites included 9 monohydroxylated metabolites, 1 demethylated metabolite, 7 demethylated and monohydroxylated metabolites, 4 dihydroxylated metabolites, 1 hydration metabolite, 1 didemethylated metabolite, 2 glucosylated metabolites, 1 monohydroxylated and dehydrogenated metabolite, 2 monohydroxylated and demethylated and dehydrogenated metabolites, 2 dimerized metabolites, 3 dimerized and monohydroxylated metabolites, 2 dimerized and didemethylated metabolites, and 5 dimerized and demethylated metabolites. Finally, the major metabolic reactions of AP in rat hepatic S9 were summarized and found to be hydroxylation, demethylation, dimerization, hydration, and dehydrogenation. More importantly, the biotransformation from AP to M2 and the dimerization of AP by incubation with hepatic S9 were reported for the first time. In conclusion, this is the first report on the metabolism of a pure pterocarpan in animal tissues, and these findings will provide a solid basis for further studies on the metabolism of other pterocarpans.

关键词： Pterocarpan Astragali Radix LCMS Hepatic S9 Metabolism

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当归的化学成分指纹图谱

药学学报 2008年第7期43卷 728-732页

作者：吴燕燕尚明英蔡少青北京大学药学院天然药物学系北京100083

比较不同产地的当归样品与市售药材之间的化学成分差异,为当归的质量控制提供参考。采用高效液相色谱法测定了16个不同产地的19份全归样品及28份市售药材(除6份全归,1份归头外,其余21份均为饮片)的指纹图谱,以阿魏酸为参照,鉴定12个共... 详细信息

比较不同产地的当归样品与市售药材之间的化学成分差异,为当归的质量控制提供参考。采用高效液相色谱法测定了16个不同产地的19份全归样品及28份市售药材(除6份全归,1份归头外,其余21份均为饮片)的指纹图谱,以阿魏酸为参照,鉴定12个共有峰。结果显示,当归饮片指纹图谱共有峰数目普遍较全归样品少,共有峰吸收值除峰11、12外,其余均较全归样品的共有峰吸收值低。结合系统聚类分析、相似度计算等方法对产地收集的当归样品和商品药材的指纹图谱进行评价比较,结果发现当归全归与饮片基本可以聚成两大类。全归(y-17、s-3、s-5及s-6除外)的相似度在0.973以上,饮片的相似度则在0.969以下,表明当归全归与饮片化学成分存在较大差异。本实验结果提示为保持药材成分的稳定,当归最好以全归的形式流通,同时应该注意当归的贮藏方式及年限。

关键词：当归当归饮片指纹图谱相似度计算

中药“显效理论”或有助于阐释并弘扬中药特色优势

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中国中药杂志 2015年第17期40卷 3435-3443页

作者：蔡少青王璇尚明英徐风刘广学北京大学药学院生物学研究室北京100191 北京大学药学院化学生物学系北京100191

该文归纳出中药"显效理论",即中药通过"众多显效形式(显效型)的单靶点叠加作用、多靶点协同作用及毒性分散效应"发挥药效并削弱自身毒性。一味中药可含有约1 000种成分,一种成分口服进入体内后又可产生约100种代谢产物。无数化学成分及... 详细信息

该文归纳出中药"显效理论",即中药通过"众多显效形式(显效型)的单靶点叠加作用、多靶点协同作用及毒性分散效应"发挥药效并削弱自身毒性。一味中药可含有约1 000种成分,一种成分口服进入体内后又可产生约100种代谢产物。无数化学成分及其无数体内代谢产物中的众多显效形式可共同发挥"集团军式作用"。在药物分子少、靶点分子多的情况下,中药不同种的显效型分子可相继与靶点分子结合,发生叠加作用,当"靶点充分占位"时药效始启动。既有浓度上的叠加作用又有时间段先后的叠加作用,这使得药效得以持久。显效型呈现药效叠加和毒性分散,源于不同显效形式分子结构之间药效基团相同而毒性基团不完全相同。"毒性分散效应"适于对无毒中药而不适于对有毒中药的解释。显效理论揭示中药可以众多化学成分及众多代谢产物参与发挥药效过程,包括叠加作用、协同作用及毒性分散效应,可有助于阐释和弘扬中药特色优势。今后需研究/确证的问题:中药药效物质基础及其作用机制是怎样构成的?多数中药为什么毒性小?体现中药特色优势的中药"显效理论"如何在新药研发中应用?

关键词：中药显效理论显效形式显效型多成分单靶点叠加作用多成分多靶点协同作用毒性分散效应集团军式作用靶点分子靶点充分占位中药药效物质作用机制代谢产物

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斜茎獐牙菜化学成分指纹图谱研究

中国药学杂志 2017年第17期52卷 1493-1496页

作者：李耀利王梦达尚明英蔡少青北京大学药学院北京100191

目的研究青叶胆常见市场习用品斜茎獐牙菜的化学成分指纹图谱,并比较斜茎獐牙菜与正品青叶胆(弥勒獐牙菜)的主要成分差异,为药材品种鉴定、寻找青叶胆替代品提供依据。方法采用HPLC方法,测定了12份斜茎獐牙菜的指纹图谱,确定了13个色谱... 详细信息

目的研究青叶胆常见市场习用品斜茎獐牙菜的化学成分指纹图谱,并比较斜茎獐牙菜与正品青叶胆(弥勒獐牙菜)的主要成分差异,为药材品种鉴定、寻找青叶胆替代品提供依据。方法采用HPLC方法,测定了12份斜茎獐牙菜的指纹图谱,确定了13个色谱峰作为共有峰;运用该方法比较了斜茎獐牙菜与弥勒獐牙菜指纹图谱的差异,通过相似度评价和聚类分析对图谱数据进行分析。结果测定了12批斜茎獐牙菜样品、5批弥勒獐牙菜样品,种内和种间相似度结果均大于0.94,相似程度高。结论所测定的12批斜茎獐牙菜样品具有很高的相似度,与药典规定正品青叶胆样品也具有高的相似度,斜茎獐牙菜具有替代药典规定正品青叶胆使用的可能性。

关键词：斜茎獐牙菜青叶胆高效液相色谱法指纹图谱

桂枝汤有效成分苯丙烯类化合物干预IL-1β刺激小鼠脑微血管内皮细胞释放PGE_2的构效关系

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药学学报 2007年第7期42卷 798-802页

作者：马悦颖尚明英李沧海霍海如蔡少青姜廷良中国中医科学院中药研究所唐氏中药研究中心北京100700 北京大学药学院北京100083 中国中医科学院医学实验中心北京100700

To observe the effects of phenylallyl compounds on prostaglandin E2（PGE2）release in mouse cerebral microvascular endothelial cells （bEnd.3） stimulated by IL-1β, and to analyze their structure-activity relationship. Different concentrations of phenylallyl compounds were added separately, and the content of PGE2 induced by IL-1β in the culture media was measured by ELISA assay. The 50% inhibitory concentration （IC 50 ） of PGE2 was calculated. Studies showed that phenylallyl compounds could affect the PGE2 release differently in bEnd.3 cells induced by IL-1β. Close relationships were shown between the inhibitory activities and the location and number of the substituent groups. In conclusion, phenylallyl compounds exhibited inhibitory activities at different extent on PGE2 release in bEnd.3 cells stimulated by IL-1β and presented certain structure-activity relationship.

关键词：苯丙烯类化合物前列腺素E2 构效关系脑微血管内皮细胞白介素1 桂枝汤

Effects of carbon content on the microstructure and tensile properties of a low-density steel

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International Journal of Minerals,Metallurgy and Materials 2025年第2期32卷 391-401页

作者： Yongxuan shang mingyu Fan Shuyong Jiang Zhongwu Zhang Key Laboratory of Superlight Materials and Surface Technology Ministry of EducationCollege of Materials Science and Chemical EngineeringHarbin Engineering UniversityHarbin 150001China State Key Laboratory of Metal Material for Marine Equipment and Application Iron&Steel Research Institute of Ansteel Group CorporationAnshan 114009China

Carbon can change the phase components of low-density steels and influence the mechanical *** this study,a new method to control the carbon content and avoid the formation ofδ-ferrite by decarburization treatment was *** microstructural changes and mechanical characteristics with carbon content induced by decarburization were systematically ***-Jaoul(C-J)analysis was employed to examine the work hardening characteristics during the tensile *** decarburization by heat treatments,the carbon content within the austenite phase decreased,while Mn and Al were almost unchanged;this made the steel with full austenite transform into the austenite and ferrite dual ***,(Ti,V)C carbides existed in both matrix phase and the mole fraction almost the *** addition,the formation of other carbides *** loss induced a decrease in strength due to the weakening of the carbon solid *** the steel with the single austinite,the deformation mode of austenite was the dislocation planar glide,resulting in the formation of *** the dual-phase steel,the deformation occurred by the dislocation planar glide of austenite first,with the increase in strain,the cross slip of ferrite took place,forming dislocation cells in *** the late stage of deformation,the work hardening of austinite increased rapidly,while that of ferrite increased slightly.

关键词： low-density steels carbon content decarburization strengthening mechanisms work hardening behavior